Hydrophobic Preparations

Abstract

The present invention relates to preparations of substances in hydrophobic solvents in which they would not normally be soluble and to processes for obtaining these preparations. In particular, the invention relates to preparations of hydrophilic species in hydrophobic solvents such as oils. The use of these preparations as vaccines and in pharmaceutical compositions is also described.

1 . A single phase hydrophobic preparation comprising a hydrophilic species, and an amphiphilic component comprising sodium docusate, a phospholipid and a nonionic amphiphile, in an oil phase, wherein the moieties of the hydrophilic species are surrounded by the amphiphilic component with the hydrophilic head groups of the amphiphilic component orientated towards the hydrophilic species and wherein there is no chemical interaction between the amphiphilic component and the hydrophilic species; characterised in that said non-ionic amphiphile has a lipophilic chain comprising 10 to 20 carbons, and a head group comprising 2 to 10 oxyethylene groups or 1 to 3 hydroxyl groups. 
     
     
         2 . The preparation of  claim 1  wherein said hydrophilic species is selected from peptides, proteins, lipids, sugars, nucleic acids, steroids and/or conjugates of one or more of these agents in combination, and/or a conjugate with at least one medium- or long-chain hydrocarbon tail. 
     
     
         3 . A method of manufacture of a hydrophobic preparation containing a hydrophilic species which includes the following steps:
 Mixing a solution of sodium docusate, a phospholipid and a non-ionic amphiphile dissolved in a hydrophobic solvent with a solution of a hydrophilic species dissolved in an aqueous phase to form an emulsion,   (ii) removing the aqueous phase and hydrophobic solvent;   (iii) Adding an oil phase to the dry residue obtained in (ii).   
     
     
         4 . A method as claimed in  claim 3  wherein said hydrophobic solvent is selected from cyclohexane, cycloheptane, cyclooctane or mixtures thereof and optionally tertiary butanol. 
     
     
         5 . A method as claimed in  claim 3  wherein step (ii) is carried out by lyophilisation. 
     
     
         6 . The method of  claim 3  wherein said hydrophilic species is selected from peptides, proteins, lipids, sugars, nucleic acids, steroids and/or conjugates of one or more of these agents in combination, and/or a conjugate with at least one medium- or long-chain hydrocarbon tail. 
     
     
         7 . The method of  claim 3  wherein said hydrophilic species is collagen or fragments, derivatives and analogues thereof, which is dissolved in a mixture of acetic acid and dimethyl sulfoxide 
     
     
         8 . A two phase composition comprising an aqueous phase and a single phase hydrophobic preparation obtainable by the method of  claim 3 . 
     
     
         9 . A two phase composition of  claim 8  wherein said two phase composition is an oil-in water emulsion. 
     
     
         10 . A two phase composition of  claim 8  wherein said aqueous phase comprises gelatin or albumin. 
     
     
         11 . A two phase composition of  claim 10  wherein said two phase composition is a microcapsule. 
     
     
         12 . A method of forming a two phase composition comprising contacting a preparation obtainable by a method of  claim 3  with an aqueous solution. 
     
     
         13 . The method of  claim 12  wherein said aqueous phase comprises gelatin or albumin. 
     
     
         14 . (canceled) 
     
     
         15 . A composition comprising a preparation obtainable by a method of  claim 3  and optionally one or more pharmaceutical excipients, diluents or carriers. 
     
     
         16 . A vaccine comprising a preparation of  claim 14 . 
     
     
         17 . A vaccine of  claim 16  adapted for oral administration. 
     
     
         18 . A vaccine of  claim 17  comprising a capsule. 
     
     
         19 . (canceled) 
     
     
         20 . The vaccine of  claim 16  wherein said composition comprises a malaria antigen or an influenza antigen, or an enteric disease pathogen antigen. 
     
     
         21 - 22 . (canceled) 
     
     
         23 . A composition of  claim 15  comprising collagen for use in treating rheumatoid arthritis. 
     
     
         24 . A cosmetic formulation comprising a preparation obtainable by a method of  claim 3  and optionally one or more excipients, diluents or carriers.